Ru(II)-catalyzed late-stage C-H amidation of medicinally relevant benzodiazepine scaffold

A late-stage C-H functionalization of 1,4-benzodiazepines for direct C-H amidation has been developed via Ru-catalyzed C-H activation. This method efficiently generates medicinally relevant functionalized products using Ru-metal. Tosyl azide serves as a bench-stable amidating reagent. The amidated product is further converted to an aminated product through chemoselective hydrolysis of the sulfonamide bond. In mechanistic studies, ruthenacycle has been synthesized and charac-terized by NMR spectroscopy.